Assay Detail
Binding
CHEMBL828160
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Inhibition of human PDE7A1 expressed in baculovirus infected Sf9 cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
High affinity 3',5'-cyclic-AMP phosphodiesterase 7A (CHEMBL3012) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.25 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL182536 | — | — | 1 | 8.46 |
| CHEMBL184861 | — | — | 1 | 8.40 |
| CHEMBL185101 | — | — | 1 | 8.00 |
| CHEMBL427152 | — | — | 1 | 8.00 |
| CHEMBL360627 | — | — | 1 | 8.00 |
| CHEMBL365447 | — | — | 1 | 8.00 |
| CHEMBL359890 | — | — | 1 | 8.00 |
| CHEMBL183102 | — | — | 1 | 8.00 |
| CHEMBL184279 | — | — | 1 | 7.70 |
| CHEMBL185523 | — | — | 1 | 7.52 |
| CHEMBL363658 | — | — | 1 | 7.40 |
| CHEMBL183280 | — | — | 1 | 7.40 |
| CHEMBL183965 | — | — | 1 | 7.30 |
| CHEMBL363894 | — | — | 1 | 7.00 |
| CHEMBL184903 | — | — | 1 | 6.82 |
| CHEMBL185460 | — | — | 1 | 6.77 |
| CHEMBL364200 | — | — | 1 | 6.68 |
| CHEMBL184013 | — | — | 1 | 6.40 |
| CHEMBL184979 | — | — | 1 | 6.02 |
| CHEMBL185275 | — | — | 1 | 5.98 |
| CHEMBL185108 | — | — | 1 | 5.91 |
| CHEMBL184701 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL182536 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL184861 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL185101 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL427152 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL360627 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL365447 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL359890 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL183102 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL184279 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL185523 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL363658 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL183280 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL183965 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL363894 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL184903 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL185460 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL364200 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL184013 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL184979 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL185275 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL185108 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL184701 | — | IC50 | = | 1620.0 | nM | 5.79 |